2. Apoptosis
  3. IAP Apoptosis
  4. SM-164 hydrochloride

SM-164 hydrochloride 

目录号: HY-15989A 纯度: 98.10%
COA 产品使用指南

摩尔计算器

SM-164 hydrochloride 是一种可渗透细胞的 Smac 类似物。SM-164 与含有 BIR2 和 BIR3 结构域的 XIAP 蛋白结合，IC50 值为 1.39 nM，SM-164 用作 XIAP 的强效拮抗剂。

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SM-164 hydrochloride Chemical Structure

SM-164 hydrochloride Chemical Structure

CAS No. : 2734174-02-6

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥7642
In-stock
2 mg ￥2990
In-stock
5 mg ￥4200
In-stock
10 mg ￥6000
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of SM-164 hydrochloride:

SM-164 hydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 36 篇科研文献

WB

    SM-164 hydrochloride purchased from MCE. Usage Cited in: Biomed Res Int. 2019 Apr 7;2019:2121357.  [Abstract]

    The mouse alveolar epithelium cell line MLE12 is exposed to SM-164 for 24h with or without LPS for 24h. RIPK3 and MLKL are downregulated along with the inhibition of cIAP2 by SM-164 during LPS-induced ARDS.

    SM-164 hydrochloride purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Nov 15;9(12):1140.   [Abstract]

    MEF cells are transfected with indicated siRNA for 3 days and then treated with TNF+Smac+zVAD, or poly I:C+zVAD for 3 h.

    查看 IAP 亚型特异性产品:

    查看所有亚型
    cIAP cIAP-1 cIAP-2 XIAP

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SM-164 hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.

    IC50 & Target[1][2]

    cIAP-1

    0.31 nM (Ki)

    cIAP-2

    1.1 nM (Ki)

    cIAP

     

    体外研究
    (In Vitro)

    SM-164 is a non-peptide, cell-permeable, bivalent small-molecule, which mimics Smac protein for targeting XIAP. SM-164 binds to XIAP containing both BIR domains with an IC50 value of 1.39 nM, being 300 and 7000-times more potent than its monovalent counterparts and the natural Smac AVPI peptide, respectively. SM-164 concurrently interacts with both BIR domains in XIAP and functions as an ultra-potent antagonist of XIAP in both cell-free functional and cell-based assays. SM-164 targets cellular XIAP and effectively induces apoptosis at concentrations as low as 1 nM in leukemia cancer cells, while having a minimal toxicity to normal human primary cells at 10,000 nM[1]. The binding affinities of SM-164 to XIAP, cIAP-1, and cIAP-2 proteins are determined using fluorescence-polarization based assays. SM-164 has a Ki value of 0.56 nM to XIAP protein containing both BIR2 and BIR3 domains. SM-164 has a Ki value of 0.31 nM to cIAP-1 protein containing both BIR2 and BIR3 domains. SM-164 binds to cIAP-2 BIR3 protein with Ki values of 1.1 nM. Addition of exogenous TNFα can significantly enhance the activity of these Smac mimetics, especially for SM-164, in resistant cancer cell lines such as HCT116 and MDA-MB-453[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    SM-164 hydrochloride 相关抗体:
    体内研究
    (In Vivo)

    SM-164 is evaluated for its ability to inhibit tumor growth. SM-164 is highly effective in inhibition of tumor growth and capable of achieving tumor regression in the MDA-MB-231 xenograft model. Treatment with SM-164 at 1 mg/kg completely inhibits tumor growth during the treatment. Treatment with SM-164 at 5 mg/kg reduces the tumor volume from 147±54 mm3 at the beginning of the treatment (day 25) to 54±32 mm3 at the end of the treatment (day 36), a reduction of 65%. The strong antitumor activity by SM-164 is long lasting and not transient. SM-164 at 5 mg/kg is statistically more effective than Taxotere at the end of the treatment (P<0.01) or when the tumor size in the control group reaches 750 mm3 (P<0.02)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    1157.88

    Formula

    C62H85ClN14O6
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    H2O 中的溶解度 : ≥ 106 mg/mL (91.55 mM)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 0.8636 mL 4.3182 mL 8.6365 mL
    5 mM 0.1727 mL 0.8636 mL 1.7273 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： PBS

      Solubility: 50 mg/mL (43.18 mM); 澄清溶液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料
    参考文献
    Kinase Assay
    [2]

    A set of sensitive and quantitative fluorescence polarization (FP)-based assays are developed to determine the binding affinities of our designed Smac mimetics to XIAP BIR3, XIAP containing both BIR2 and BIR3 domains, cIAP-1 BIR3, cIAP-1 containing both BIR2 and BIR3 domains, and cIAP-2 protein. The FP-based assay for XIAP BIR3 protein is measured. Briefly, 5-carboxyfluorescein is coupled to the lysine side chain of a mutated Smac peptide with the sequence (AbuRPFK-Fam) and this fluorescently tagged peptide (named SM5F) is used as the fluorescent tracer in FP-based binding assay to XIAP BIR3. The Kd value of this fluorescent tracer is determined to be 17.9 nM to XIAP BIR3. In competitive binding experiments, a tested compound is incubated with 30 nM of XIAP BIR3 protein and 5 nM of SM5F in the assay buffer (100 mM potassium phosphate, pH 7.5; 100μg/mL bovine gamma globulin; 0.02 % sodium azide)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [2]

    HCT116 colon cancer cells are treated with SM-164 (1, 10, and 100 nM) alone, TNFα alone, or the combination for 48 h. Cell growth inhibition is determined by a WST assay[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    SCID mice (8-10 per group) bearing MDA-MB-231 xenograft tumors are treated i.v. with 1 and 5 mg/kg of SM-164 or 7.5 mg/kg of Taxotere or vehicle control daily, 5 d/wk for 2 wk. Tumor sizes and animal weights are measured thrice a week[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    SM-164 hydrochloride 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 0.8636 mL 4.3182 mL 8.6365 mL 21.5912 mL
    5 mM 0.1727 mL 0.8636 mL 1.7273 mL 4.3182 mL
    10 mM 0.0864 mL 0.4318 mL 0.8636 mL 2.1591 mL
    15 mM 0.0576 mL 0.2879 mL 0.5758 mL 1.4394 mL
    20 mM 0.0432 mL 0.2159 mL 0.4318 mL 1.0796 mL
    25 mM 0.0345 mL 0.1727 mL 0.3455 mL 0.8636 mL
    30 mM 0.0288 mL 0.1439 mL 0.2879 mL 0.7197 mL
    40 mM 0.0216 mL 0.1080 mL 0.2159 mL 0.5398 mL
    50 mM 0.0173 mL 0.0864 mL 0.1727 mL 0.4318 mL
    60 mM 0.0144 mL 0.0720 mL 0.1439 mL 0.3599 mL
    80 mM 0.0108 mL 0.0540 mL 0.1080 mL 0.2699 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    SM-1642734174-02-6SM164SM 164IAPApoptosisInhibitorinhibitorinhibit

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